普马司他
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- CAS号:
- 192329-42-3
- 英文名:
- Prinomastat
- 英文别名:
- Ag3340;Ag 3340;Ag-3340;KB-R 9896;Prinomastat;AG3340 hydrochloride;AG 3340 hydrochloride;AG-3340 hydrochloride;Phenprobamate Impurity 2;Prinomastat hydrochloride
- 中文名:
- 普马司他
- 中文别名:
- 普啉司他;普马司他;化合物 T12539L;MMP抑制剂(PRINOMASTAT);(S)-2-[(羟基氨基)甲基]-5,6-二甲基-4-(4-吡啶-4-基氧苯基)磺酰基吗啉-3-硫酮
- CBNumber:
- CB01475597
- 分子式:
- C18H21N3O5S2
- 分子量:
- 423.51
- MOL File:
- 192329-42-3.mol
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普马司他化学性质
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熔点:
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149.8°
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密度:
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1.377±0.06 g/cm3(Predicted)
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储存条件:
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room temp
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溶解度:
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H2O: soluble15mg/mL (clear solution)
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形态:
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powder
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酸度系数(pKa):
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9.25±0.23(Predicted)
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颜色:
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white to beige
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普马司他性质、用途与生产工艺
Prinomastat (AG3340) 是一种广谱，有效的口服活性金属蛋白酶 (MMP) 抑制剂，对于 MMP-1, MMP-3 和 MMP-9 的 IC50 分别为 79 nM，6.3 nM 和 5.0 nM。Prinomastat 抑制 MMP-2, MMP-3 和 MMP-9 的 Ki 分别为 0.05 nM，0.3 nM 和 0.26 nM。Prinomastat 穿过血脑屏障。抗肿瘤活性。
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MMP-9
5 nM (IC
50
)
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MMP-9
0.26 nM (Ki)
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MMP-2
0.05 nM (Ki)
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MMP-1
79 nM (IC
50
)
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MMP-3
6..3 nM (IC
50
)
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MMP-3
0.3 nM (Ki)
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Prinomastat (AG3340; 0.1-1 µg/mL; 4 days; C57MG/Wnt1 cells) inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and β-catenin transcriptional activity by Prinomastat.
Co-culture of L/Wnt3a cells and CT7 cells increases the Topflash activity in CT7 cells, and co-culturing both L/Wnt3a cells and MMP-3 overexpressing C57MG cells with CT7 cells increases the Topflash luciferase activity in CT7 cells beyond the level observed with L/Wnt3a cells, and these effects are all suppressed by Prinomastat (AG3340).
Inhibition of entry of C57MG/Wnt1 cells into S phase by Prinomastat corresponds to a decrease in expression of cyclin D1 and Erk1/2 phosphorylation. The effect of Prinomastat on Wnt1-induced migration is then examined using an in vitro wound assay. As anticipated, the migration of C57MG/Wnt1 cells is increased by 1.8-fold when compared with C57MG cells.The effect of Wnt1 on the cellular distribution of vimentin is reversed by Prinomastat in C57MG/Wnt1 cells.
Western Blot Analysis
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Cell Line:
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C57MG/Wnt1 cells
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Concentration:
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0.1 µg/mL, 1 µg/mL
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Incubation Time:
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4 days
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Result:
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A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells.
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In a human fibrosarcoma mouse model (HT1080), the mice are treated therapeutically for 14-16 days with 50 mg/kg/day ip daily starting day 3 to 6 after tumour inoculation. Prinomastat is well tolerated by the animals, and there are no signs of weight loss or other adverse effects. Prinomastat has good tumour growth inhibition, with a short T
1/2
of 1.6 hours.
普马司他
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-12170A | 普马司他
Prinomastat hydrochloride | 192329-42-3 | 1mg | 1250元 |
| 2024/01/25 | HY-12170A | 普马司他
Prinomastat hydrochloride | 192329-42-3 | 5mg | 3750元 |
192329-42-3, 普马司他 相关搜索:
- 细胞生物学试剂
- 化合物 T12539L
- 普啉司他
- MMP抑制剂(PRINOMASTAT)
- (S)-2-[(羟基氨基)甲基]-5,6-二甲基-4-(4-吡啶-4-基氧苯基)磺酰基吗啉-3-硫酮
- 普马司他
- 192329-42-3
- Phenprobamate Impurity 2
- 3-Thiomorpholinecarboxamide, N-hydroxy-2,2-dimethyl-4-[[4-(4-pyridinyloxy)phenyl]sulfonyl]-, (3S)-
- (3S)-N-hydroxy-2,2-dimethyl-4-[4-(pyridin-4-yloxy) benzenesulfonyl]thiomorpholine-3-carboxamide
- Prinomastat hydrochloride
- AG-3340 hydrochloride
- Prinomastat
- (S)-2-[(Hydroxyamino)methyl]-5,6-dimethyl-4-(4-pyridin-4-yloxyphenyl)sulfonylmorpholine-3-thione
- 2-[(hydroxyamino)methyl]-5,6-dimethyl-4-(4-pyridin-4-yloxyphenyl)sulfonyl-morpholine-3-thione
- AG3340 hydrochloride
- AG 3340 hydrochloride
- (S)-2,2-Dimethyl-4-((p-(4-pyridyloxy)phenyl)sulfonyl)-3-thiomorpholinecarbohydroxamic acid hydrochloride
- KB-R 9896
- Ag-3340
- Ag3340
- Ag 3340
- 3-Thiomorpholinecarboxamide, N-hydroxy-2,2-dimethyl-4-((4-(4-pyridinyloxy)phenyl)sulfonyl)-, (S)-
- (S)-2,2-DIMETHYL-N-HYDROXY-4-[4-(4-PYRIDYLOXY)PHENYLSULFONYL]-1,4-THIAZINANE-3-CARBOXAMIDE